Background: This study aims to evaluate the safety and efficacy of Xuezhikang in the treatment of unstable angina pectoris (UAP) in patients with elevated liver enzymes caused by statins. Methods: Ninety UAP patientswith elevated liver enzymes (higher than 3-fold the upper limits of normal caused by statins) were randomly divided into 3 groups: withdrawal of simvastatin (group A), continued taking of simvastatin (group B) and switching to Xuezhikang capsules (group C). Results: Blood lipids and high-sensitivity C-reactive protein (hs-CRP) were measured before and after treatment, and liver enzymes were measured every two weeks. As the liver enzymes of the patients in group A returned to normal, they could again undertake administration of simvastatin. If the liver enzyme levels remained abnormal at four weeks, polyene phosphatidylcholine would be added. The endpoint events of each group were followed-up. After treatment for 4 weeks, the liver enzymes decreased in all of the three groups and there was a significant difference (p < 0.05). However, at 8 weeks the liver enzymes showed no significant difference among the three groups (p > 0.05). The blood lipids and hs-CRP were both reduced in group B and C. The decreased triglyceride and hs-CRP levels and increased high-density lipoprotein cholesterol level in group C weremore remarkable than those in group B (p < 0.05). The incidence rate of endpoint events in group A was the highest (p < 0.05) among the three groups. Conclusions: Xuezhikang is safe and effective in the treatment for UAP patients with elevated liver enzymes caused by statins.